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Structure‐Function Analyses of Eicosanoid Receptors: Physiologic and Therapeutic Implications
Author(s) -
BREYER RICHARD M.,
KENNEDY CHRISTOPHER R. J.,
ZHANG YAHUA,
BREYER MATTHEW D.
Publication year - 2000
Publication title -
annals of the new york academy of sciences
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.712
H-Index - 248
eISSN - 1749-6632
pISSN - 0077-8923
DOI - 10.1111/j.1749-6632.2000.tb06552.x
Subject(s) - receptor , prostaglandin e2 receptor , eicosanoid , inflammation , prostaglandin , biology , endocrinology , lipid signaling , medicine , microbiology and biotechnology , pharmacology , agonist , arachidonic acid , biochemistry , immunology , enzyme
A bstract : Prostaglandins (PGs) are ubiquitous lipid mediators derived from cyclooxygenase (COX) metabolism of arachidonic acid that exert a broad range of physiologic activities including modulation of inflammation, ovulation, and arterial blood pressure. The physiologic actions of PGs are mediated in part by their interaction with specific G‐protein‐coupled PG receptors. Eight PG receptors have been cloned, including four for the major COX metabolite, PGE 2 . The physiologic roles of the PGE 2 receptors have been investigated utilizing subtype‐selective agonists, localization of receptor mRNA expression, and creation of mice with targeted disruption of PG receptor genes. These analyses have delineated discrete roles for the various PG receptor subtypes. Recent studies on mice lacking the PGE 2 EP 2 receptor have implicated the PGE 2 EP 2 receptor subtype in arterial dilatation and salt‐sensitive hypertension, and also indicate that this receptor plays a key role in female fertility. The EP 2 receptor may thus prove to be a productive target for pharmacological intervention in the treatment of hypertension and infertility.